CN102548983B - 作为单酰甘油脂肪酶抑制剂的杂芳族和芳族哌嗪基氮杂环丁基酰胺 - Google Patents
作为单酰甘油脂肪酶抑制剂的杂芳族和芳族哌嗪基氮杂环丁基酰胺 Download PDFInfo
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- CN102548983B CN102548983B CN201080028748.2A CN201080028748A CN102548983B CN 102548983 B CN102548983 B CN 102548983B CN 201080028748 A CN201080028748 A CN 201080028748A CN 102548983 B CN102548983 B CN 102548983B
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- pyridine
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Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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| US17166009P | 2009-04-22 | 2009-04-22 | |
| US61/171660 | 2009-04-22 | ||
| PCT/US2010/032098 WO2010124121A1 (en) | 2009-04-22 | 2010-04-22 | Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitor |
Publications (2)
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| CN102548983A CN102548983A (zh) | 2012-07-04 |
| CN102548983B true CN102548983B (zh) | 2014-09-17 |
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| EP (1) | EP2421852B9 (pt) |
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| CN (1) | CN102548983B (pt) |
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| AU (1) | AU2010238745A1 (pt) |
| BR (1) | BRPI1014888A2 (pt) |
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| RU (1) | RU2558141C2 (pt) |
| TW (1) | TWI495637B (pt) |
| WO (1) | WO2010124121A1 (pt) |
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| TW201105655A (en) | 2009-04-22 | 2011-02-16 | Janssen Pharmaceutica Nv | Azetidinyl diamides as monoacylglycerol lipase inhibitors |
| RU2013114771A (ru) | 2010-09-03 | 2014-10-10 | Янссен Фармацевтика Нв | Диамиды азетидинила как ингибиторы моноацилглицерол липазы |
| JP2013537920A (ja) * | 2010-09-27 | 2013-10-07 | ヤンセン ファーマシューティカ エヌ．ベー． | モノアシルグリセロールリパーゼ阻害剤としてのオキソピペラジン−アゼチジンアミド及びオキソジアゼピン−アゼチジンアミド |
| US8575363B2 (en) | 2010-10-22 | 2013-11-05 | Janssen Pharmaceutica N.V. | Amino-pyrrolidine-azetidine diamides as monoacylglycerol lipase inhibitors |
| US8513423B2 (en) | 2010-10-22 | 2013-08-20 | Janssen Pharmaceutica, Nv | Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors |
| WO2015099196A1 (en) | 2013-12-26 | 2015-07-02 | Takeda Pharmaceutical Company Limited | 4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (magl) inhibitors |
| AU2015264336B2 (en) | 2014-05-19 | 2018-08-30 | Boehringer Ingelheim Animal Health USA Inc. | Anthelmintic compounds |
| WO2016158956A1 (ja) | 2015-03-30 | 2016-10-06 | 武田薬品工業株式会社 | 複素環化合物 |
| WO2017023861A1 (en) | 2015-08-03 | 2017-02-09 | The Regents Of The University Of California | Compositions and methods for modulating abhd2 activity |
| US10463753B2 (en) | 2016-02-19 | 2019-11-05 | Lundbeck La Jolla Research Center, Inc. | Radiolabeled monoacylglycerol lipase occupancy probe |
| JP6832342B2 (ja) | 2016-03-31 | 2021-02-24 | 武田薬品工業株式会社 | 複素環化合物 |
| DK3436444T3 (da) | 2016-03-31 | 2020-07-27 | Takeda Pharmaceuticals Co | Heterocyklisk forbindelse |
| BR112020005720A2 (pt) | 2017-09-29 | 2020-10-20 | Takeda Pharmaceutical Company Limited | composto ou sal, medicamento, métodos para inibir monoacilglicerol lipase e para a profilaxia ou o tratamento de doença de alzheimer, doença de parkinson, doença de huntington, esclerose lateral amiotrófica, esclerose múltipla, distúrbio de ansiedade, dor, epilepsia ou depressão, e, uso do composto ou sal. |
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|---|---|---|---|---|
| PE20020507A1 (es) * | 2000-10-17 | 2002-06-25 | Schering Corp | Compuestos no-imidazoles como antagonistas del receptor histamina h3 |
| DE60312042T2 (de) * | 2002-12-23 | 2007-10-31 | Janssen Pharmaceutica N.V. | Substituierte 1-piperidin-4-yl-4-azetidin-3-yl-piperazinderivate und deren verwendung als neurokininantagonisten |
| EP1702916A1 (en) * | 2005-03-18 | 2006-09-20 | Santhera Pharmaceuticals (Schweiz) GmbH | DPP-IV inhibitors |
| FR2915199B1 (fr) * | 2007-04-18 | 2010-01-22 | Sanofi Aventis | Derives de triazolopyridine-carboxamides et triazolopyrimidine-carboxamides, leur preparation et leur application en therapeutique. |
| EP2283126A1 (en) * | 2008-04-25 | 2011-02-16 | Janssen Pharmaceutica, N.V. | Crystal structure of monoacylglycerol lipase (mgll) |
| EP2283127B1 (en) * | 2008-04-25 | 2015-04-08 | Janssen Pharmaceutica, N.V. | Protein engineering of monoacylglycerol lipase (mgll) |
| EP2180048B1 (en) * | 2008-10-09 | 2014-12-17 | Janssen Pharmaceutica N.V. | Alternative crystal form of monoacylglycerol lipase (MGLL) |
| US8435977B2 (en) * | 2009-04-22 | 2013-05-07 | Janssen Pharmaceutica, Nv | Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors |
-
2010
- 2010-04-22 DK DK10719479.7T patent/DK2421852T3/da active
- 2010-04-22 EP EP10719479.7A patent/EP2421852B9/en active Active
- 2010-04-22 TW TW099112744A patent/TWI495637B/zh not_active IP Right Cessation
- 2010-04-22 RU RU2011147203/04A patent/RU2558141C2/ru not_active IP Right Cessation
- 2010-04-22 CN CN201080028748.2A patent/CN102548983B/zh not_active Expired - Fee Related
- 2010-04-22 CA CA2759714A patent/CA2759714A1/en not_active Abandoned
- 2010-04-22 PT PT107194797T patent/PT2421852E/pt unknown
- 2010-04-22 AR ARP100101336A patent/AR076375A1/es not_active Application Discontinuation
- 2010-04-22 ES ES10719479.7T patent/ES2486674T3/es active Active
- 2010-04-22 WO PCT/US2010/032098 patent/WO2010124121A1/en active Application Filing
- 2010-04-22 AU AU2010238745A patent/AU2010238745A1/en not_active Abandoned
- 2010-04-22 KR KR1020117027425A patent/KR20120014154A/ko not_active Application Discontinuation
- 2010-04-22 JP JP2012507394A patent/JP2012524809A/ja active Pending
- 2010-04-22 BR BRPI1014888A patent/BRPI1014888A2/pt not_active IP Right Cessation
-
2011
- 2011-10-23 IL IL215796A patent/IL215796A/en not_active IP Right Cessation
-
2012
- 2012-07-31 HK HK12107498.8A patent/HK1166794A1/xx not_active IP Right Cessation
- 2012-11-01 HK HK12111003.8A patent/HK1170239A1/xx not_active IP Right Cessation
-
2013
- 2013-03-04 US US13/784,036 patent/US8815839B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| IL215796A0 (en) | 2012-01-31 |
| US20130184251A1 (en) | 2013-07-18 |
| RU2558141C2 (ru) | 2015-07-27 |
| US8815839B2 (en) | 2014-08-26 |
| IL215796A (en) | 2015-04-30 |
| HK1166794A1 (en) | 2012-11-09 |
| JP2012524809A (ja) | 2012-10-18 |
| PT2421852E (pt) | 2014-07-31 |
| BRPI1014888A2 (pt) | 2019-09-24 |
| TWI495637B (zh) | 2015-08-11 |
| ES2486674T3 (es) | 2014-08-19 |
| TW201103917A (en) | 2011-02-01 |
| HK1170239A1 (en) | 2013-02-22 |
| WO2010124121A8 (en) | 2012-03-08 |
| AU2010238745A1 (en) | 2011-11-10 |
| RU2011147203A (ru) | 2013-05-27 |
| EP2421852A1 (en) | 2012-02-29 |
| WO2010124121A1 (en) | 2010-10-28 |
| EP2421852B9 (en) | 2015-07-01 |
| EP2421852B1 (en) | 2014-05-21 |
| AR076375A1 (es) | 2011-06-08 |
| DK2421852T3 (da) | 2014-08-18 |
| CN102548983A (zh) | 2012-07-04 |
| CA2759714A1 (en) | 2010-10-28 |
| KR20120014154A (ko) | 2012-02-16 |
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